JP2020066629A5 - - Google Patents
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- Publication number
- JP2020066629A5 JP2020066629A5 JP2019189151A JP2019189151A JP2020066629A5 JP 2020066629 A5 JP2020066629 A5 JP 2020066629A5 JP 2019189151 A JP2019189151 A JP 2019189151A JP 2019189151 A JP2019189151 A JP 2019189151A JP 2020066629 A5 JP2020066629 A5 JP 2020066629A5
- Authority
- JP
- Japan
- Prior art keywords
- disease
- cancer
- crystalline form
- methylpiperidin
- pyrrolo
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 201000010099 disease Diseases 0.000 claims 11
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- CBRJPFGIXUFMTM-WDEREUQCSA-N N1=CN=C(C2=C1NC=C2)N[C@@H]2CC[C@@H](N(C2)C(C=C)=O)C Chemical compound N1=CN=C(C2=C1NC=C2)N[C@@H]2CC[C@@H](N(C2)C(C=C)=O)C CBRJPFGIXUFMTM-WDEREUQCSA-N 0.000 claims 4
- 230000001363 autoimmune Effects 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 claims 4
- 238000005481 NMR spectroscopy Methods 0.000 claims 3
- 238000001069 Raman spectroscopy Methods 0.000 claims 3
- 206010046851 Uveitis Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 230000001684 chronic Effects 0.000 claims 3
- LVOICKNPHXSSQM-UHFFFAOYSA-N prop-2-en-1-one Chemical compound C=C[C]=O LVOICKNPHXSSQM-UHFFFAOYSA-N 0.000 claims 3
- 239000007787 solid Substances 0.000 claims 3
- 239000000126 substance Substances 0.000 claims 3
- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 claims 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 206010012601 Diabetes mellitus Diseases 0.000 claims 2
- 206010013774 Dry eye Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 206010023332 Keratitis Diseases 0.000 claims 2
- JOXIMZWYDAKGHI-UHFFFAOYSA-N P-Toluenesulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 2
- 241000721454 Pemphigus Species 0.000 claims 2
- 206010039073 Rheumatoid arthritis Diseases 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- WEVYAHXRMPXWCK-UHFFFAOYSA-N acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 2
- 230000001154 acute Effects 0.000 claims 2
- 201000004384 alopecia Diseases 0.000 claims 2
- 231100000360 alopecia Toxicity 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 201000004624 dermatitis Diseases 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 210000000056 organs Anatomy 0.000 claims 2
- KJIFKLIQANRMOU-UHFFFAOYSA-N oxidanium;4-methylbenzenesulfonate Chemical compound O.CC1=CC=C(S(O)(=O)=O)C=C1 KJIFKLIQANRMOU-UHFFFAOYSA-N 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 201000004681 psoriasis Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000011780 sodium chloride Substances 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 201000010874 syndrome Diseases 0.000 claims 2
- 201000006704 ulcerative colitis Diseases 0.000 claims 2
- -1 7H-pyrrolo[2,3-d]pyrimidin-4-yl Chemical group 0.000 claims 1
- JJTNLWSCFYERCK-UHFFFAOYSA-N 7H-pyrrolo[2,3-d]pyrimidine Chemical compound N1=CN=C2NC=CC2=C1 JJTNLWSCFYERCK-UHFFFAOYSA-N 0.000 claims 1
- 206010000880 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000002205 Allergic Conjunctivitis Diseases 0.000 claims 1
- 208000004631 Alopecia Areata Diseases 0.000 claims 1
- 206010001897 Alzheimer's disease Diseases 0.000 claims 1
- 206010002026 Amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 208000009094 Anemia, Hemolytic, Autoimmune Diseases 0.000 claims 1
- 206010002556 Ankylosing spondylitis Diseases 0.000 claims 1
- 206010002855 Anxiety Diseases 0.000 claims 1
- 206010057666 Anxiety disease Diseases 0.000 claims 1
- 208000006673 Asthma Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 208000004300 Atrophic Gastritis Diseases 0.000 claims 1
- 208000005783 Autoimmune Thyroiditis Diseases 0.000 claims 1
- 206010003816 Autoimmune disease Diseases 0.000 claims 1
- 206010050245 Autoimmune thrombocytopenia Diseases 0.000 claims 1
- 206010004161 Basedow's disease Diseases 0.000 claims 1
- 208000009137 Behcet Syndrome Diseases 0.000 claims 1
- 201000008335 Behcet's disease Diseases 0.000 claims 1
- 206010004661 Biliary cirrhosis primary Diseases 0.000 claims 1
- 206010004938 Bipolar disease Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000008581 Brain Disease Diseases 0.000 claims 1
- 210000000481 Breast Anatomy 0.000 claims 1
- 208000000594 Bullous Pemphigoid Diseases 0.000 claims 1
- 206010006895 Cachexia Diseases 0.000 claims 1
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 1
- 206010009839 Coeliac disease Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010010741 Conjunctivitis Diseases 0.000 claims 1
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- 210000004087 Cornea Anatomy 0.000 claims 1
- 206010070976 Craniocerebral injury Diseases 0.000 claims 1
- 206010011401 Crohn's disease Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010012818 Diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 208000005679 Eczema Diseases 0.000 claims 1
- 206010014599 Encephalitis Diseases 0.000 claims 1
- 206010014623 Encephalopathy Diseases 0.000 claims 1
- 206010014625 Encephalopathy Diseases 0.000 claims 1
- 206010060742 Endocrine ophthalmopathy Diseases 0.000 claims 1
- 206010015037 Epilepsy Diseases 0.000 claims 1
- 208000009745 Eye Disease Diseases 0.000 claims 1
- 206010017860 Gastritis atrophic Diseases 0.000 claims 1
- 208000005017 Glioblastoma Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010018651 Graft versus host disease Diseases 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 claims 1
- 208000003807 Graves Disease Diseases 0.000 claims 1
- 201000004779 Graves' disease Diseases 0.000 claims 1
- 208000001204 Hashimoto Disease Diseases 0.000 claims 1
- 208000006454 Hepatitis Diseases 0.000 claims 1
- 201000001971 Huntington's disease Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010021972 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010022114 Injury Diseases 0.000 claims 1
- 206010022941 Iridocyclitis Diseases 0.000 claims 1
- 208000007766 Kaposi Sarcoma Diseases 0.000 claims 1
- 208000009319 Keratoconjunctivitis Sicca Diseases 0.000 claims 1
- 206010024324 Leukaemias Diseases 0.000 claims 1
- 208000007046 Leukemia, Myeloid, Acute Diseases 0.000 claims 1
- 208000002741 Leukoplakia Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025135 Lupus erythematosus Diseases 0.000 claims 1
- 206010057840 Major depression Diseases 0.000 claims 1
- 206010025650 Malignant melanoma Diseases 0.000 claims 1
- 210000002264 Mammary Glands, Animal Anatomy 0.000 claims 1
- 210000004293 Mammary Glands, Human Anatomy 0.000 claims 1
- 208000008585 Mastocytosis Diseases 0.000 claims 1
- 206010027480 Metastatic malignant melanoma Diseases 0.000 claims 1
- 210000000214 Mouth Anatomy 0.000 claims 1
- 206010028417 Myasthenia gravis Diseases 0.000 claims 1
- 206010028576 Myeloproliferative disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010029113 Neovascularisation Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 208000008443 Pancreatic Carcinoma Diseases 0.000 claims 1
- 206010061536 Parkinson's disease Diseases 0.000 claims 1
- 206010034277 Pemphigoid Diseases 0.000 claims 1
- 206010034695 Pernicious anaemia Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010036774 Proctitis Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000003251 Pruritus Diseases 0.000 claims 1
- 208000002098 Purpura, Thrombocytopenic, Idiopathic Diseases 0.000 claims 1
- 206010038294 Reiter's syndrome Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010038683 Respiratory disease Diseases 0.000 claims 1
- 206010039705 Scleritis Diseases 0.000 claims 1
- 206010039911 Seizure Diseases 0.000 claims 1
- 206010040070 Septic shock Diseases 0.000 claims 1
- 206010040767 Sjogren's syndrome Diseases 0.000 claims 1
- 208000008513 Spinal Cord Injury Diseases 0.000 claims 1
- 206010041823 Squamous cell carcinoma Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010042742 Sympathetic ophthalmia Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 210000001744 T-Lymphocytes Anatomy 0.000 claims 1
- 206010043709 Thyroid disease Diseases 0.000 claims 1
- 206010043778 Thyroiditis Diseases 0.000 claims 1
- 208000005765 Traumatic Brain Injury Diseases 0.000 claims 1
- 208000007979 Treatment-Resistant Depressive Disorder Diseases 0.000 claims 1
- 206010068760 Ulcers Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 206010047642 Vitiligo Diseases 0.000 claims 1
- 201000011186 acute T cell leukemia Diseases 0.000 claims 1
- 230000001058 adult Effects 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 claims 1
- 201000009596 autoimmune hypersensitivity disease Diseases 0.000 claims 1
- 201000006474 brain ischemia Diseases 0.000 claims 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- 230000002612 cardiopulmonary Effects 0.000 claims 1
- 210000004027 cells Anatomy 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 238000010276 construction Methods 0.000 claims 1
- 231100000406 dermatitis Toxicity 0.000 claims 1
- 230000001079 digestive Effects 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 231100001003 eczema Toxicity 0.000 claims 1
- 201000002491 encephalomyelitis Diseases 0.000 claims 1
- 201000001564 eosinophilic gastroenteritis Diseases 0.000 claims 1
- 201000011240 frontotemporal dementia Diseases 0.000 claims 1
- 230000002496 gastric Effects 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 239000011630 iodine Substances 0.000 claims 1
- 201000010666 keratoconjunctivitis Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000006512 mast cell neoplasm Diseases 0.000 claims 1
- 230000001404 mediated Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 201000009251 multiple myeloma Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000002077 muscle cancer Diseases 0.000 claims 1
- 201000002481 myositis Diseases 0.000 claims 1
- 201000008383 nephritis Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 230000003959 neuroinflammation Effects 0.000 claims 1
- 230000000414 obstructive Effects 0.000 claims 1
- 201000005737 orchitis Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 201000006292 polyarteritis nodosa Diseases 0.000 claims 1
- 201000008839 post-traumatic stress disease Diseases 0.000 claims 1
- 201000002728 primary biliary cirrhosis Diseases 0.000 claims 1
- 201000007914 proliferative diabetic retinopathy Diseases 0.000 claims 1
- 230000001823 pruritic Effects 0.000 claims 1
- 230000002685 pulmonary Effects 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 238000003756 stirring Methods 0.000 claims 1
- 230000002889 sympathetic Effects 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 201000009594 systemic scleroderma Diseases 0.000 claims 1
- 125000005425 toluyl group Chemical group 0.000 claims 1
- 231100000397 ulcer Toxicity 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- 238000002689 xenotransplantation Methods 0.000 claims 1
- 125000005023 xylyl group Chemical group 0.000 claims 1
- QRZXLCPZJWWANB-DTWKUNHWSA-N C[C@@H](CC1)NC[C@@H]1Nc1ncnc2c1cc[nH]2 Chemical compound C[C@@H](CC1)NC[C@@H]1Nc1ncnc2c1cc[nH]2 QRZXLCPZJWWANB-DTWKUNHWSA-N 0.000 description 1
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201862748628P | 2018-10-22 | 2018-10-22 | |
US62/748628 | 2018-10-22 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2020066629A JP2020066629A (ja) | 2020-04-30 |
JP2020066629A5 true JP2020066629A5 (zh) | 2020-07-27 |
JP6944496B2 JP6944496B2 (ja) | 2021-10-06 |
Family
ID=68343187
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2019189151A Active JP6944496B2 (ja) | 2018-10-22 | 2019-10-16 | ピロロ[2,3−d]ピリミジントシル酸塩、その結晶形態、ならびにその製造方法および中間体 |
Country Status (15)
Country | Link |
---|---|
US (1) | US20210387989A1 (zh) |
EP (1) | EP3870584A1 (zh) |
JP (1) | JP6944496B2 (zh) |
KR (1) | KR102629132B1 (zh) |
CN (1) | CN112888691B (zh) |
AR (1) | AR116797A1 (zh) |
AU (1) | AU2019363840B2 (zh) |
BR (1) | BR112021007568A2 (zh) |
CA (1) | CA3059000A1 (zh) |
IL (1) | IL282446B2 (zh) |
MX (1) | MX2021003241A (zh) |
SG (1) | SG11202103667QA (zh) |
TW (1) | TWI729530B (zh) |
WO (1) | WO2020084435A1 (zh) |
ZA (1) | ZA202101735B (zh) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP4021452B1 (en) * | 2019-08-26 | 2023-12-20 | Chemwerth Inc | Substituted (7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino compounds useful as jak1 inhibitors |
CN113121539A (zh) * | 2019-12-31 | 2021-07-16 | 江苏艾立康医药科技有限公司 | 一种pf06651600的制备方法 |
CN115023221B (zh) * | 2019-12-31 | 2024-05-28 | 辉瑞英国研发有限公司 | 1-((2s,5r)-5-((7h-吡咯并[2,3-d]嘧啶-4-基)氨基)-2-甲基哌啶-1-基)丙-2-烯-1-酮的稳定立即释放片剂和胶囊制剂 |
CN114835715B (zh) * | 2020-06-15 | 2024-04-05 | 江苏艾立康医药科技有限公司 | Pf-06651600马来酸盐及其制备方法 |
CN111732591B (zh) * | 2020-06-15 | 2022-06-10 | 江苏艾立康医药科技有限公司 | Pf-06651600 l-酒石酸盐,晶型及其制备方法 |
CN111620880B (zh) * | 2020-06-15 | 2022-06-10 | 江苏艾立康医药科技有限公司 | Pf-06651600 dl-酒石酸盐,晶型及其制备方法 |
WO2022012587A1 (zh) * | 2020-07-14 | 2022-01-20 | 苏州晶云药物科技股份有限公司 | 丙烯酮类化合物的丙二酸盐晶型及其制备方法 |
KR102473645B1 (ko) * | 2020-08-28 | 2022-12-05 | (주)부흥산업사 | (2S,5R)-벤질 5-(t-부톡시카르보닐아미노)-2-메틸피페리딘-1-카르복실레이트의 제조방법 |
CN112877379B (zh) * | 2021-01-18 | 2023-09-01 | 华南理工大学 | 一种化学酶法合成n-[(3r,6r)-6-甲基哌啶-3-基]氨基甲酸叔丁酯的方法 |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PT3077395T (pt) * | 2013-12-05 | 2018-01-03 | Pfizer | Pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinilo e pirrolo[2,3-d]piridinilo acrilamidas |
MA41350A (fr) * | 2015-01-14 | 2017-11-21 | Janssen Pharmaceutica Nv | Synthèse d'un inhibiteur de la tyrosine kinase de bruton |
CN105859721B (zh) * | 2015-01-22 | 2018-04-17 | 浙江京新药业股份有限公司 | 一种伊布鲁替尼的制备方法 |
-
2019
- 2019-10-16 JP JP2019189151A patent/JP6944496B2/ja active Active
- 2019-10-17 TW TW108137470A patent/TWI729530B/zh active
- 2019-10-17 CA CA3059000A patent/CA3059000A1/en active Pending
- 2019-10-21 KR KR1020217015125A patent/KR102629132B1/ko active IP Right Grant
- 2019-10-21 CN CN201980069164.0A patent/CN112888691B/zh active Active
- 2019-10-21 WO PCT/IB2019/058940 patent/WO2020084435A1/en active Application Filing
- 2019-10-21 AU AU2019363840A patent/AU2019363840B2/en active Active
- 2019-10-21 EP EP19794259.2A patent/EP3870584A1/en active Pending
- 2019-10-21 SG SG11202103667QA patent/SG11202103667QA/en unknown
- 2019-10-21 US US17/286,018 patent/US20210387989A1/en active Pending
- 2019-10-21 MX MX2021003241A patent/MX2021003241A/es unknown
- 2019-10-21 IL IL282446A patent/IL282446B2/en unknown
- 2019-10-21 BR BR112021007568-2A patent/BR112021007568A2/pt unknown
- 2019-10-22 AR ARP190103015A patent/AR116797A1/es unknown
-
2021
- 2021-03-15 ZA ZA2021/01735A patent/ZA202101735B/en unknown
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